Antifungal Drugs

Question 1

Azoles 
Action
PK
Side effects
Example

Answer 1

Action- inhibits cytochrome P45’ stops conversion of cell wall component ergosterol
PK- broad spec, rapid ab. High PB, metab liver, ex bile and urine
SE? GI upset, hepatotoxic
Eg? Imidazole

Question 2

Allylamines
Action
PK
side effects
Example

Answer 2

Action- inhibit enzyme squalene epoxidase, no ergosterol
PK- high PB, fungalstatic or cidal, met liver ex urine
Effective against mallezzia and dermoatophytosis
SE? Uncommon- GI upset
Eg terbinfine (ear drops)

Question 3

Polyenes 
Action
PK
Side effects
Example

Answer 3

Action-binds to ergosterol, causes leakage. Synergistic with azoles- reduces dose and toxicity
PK- fungistatic, high PB, IV infusion
SE- nephrotoxicity, hypokaleamia, hypotension
Eg- amphotericin B

Question 4

DNA/RNA inhibitors
Action
Example

Answer 4

Action- gluconsynthase inhibitors- cell wall component found only in fungi (humans only)
Eg flucytosine

Question 5

Mitotic inhibitors
Action
PK?
Side effects
Example

Answer 5

Action- binds to tubulin to stop microtubule formation. Disrupts mitosis
PK? Fungistatic, only treats superficial mycoses
SE- not for preg or lact animals. GI upset, hepatotoxicity, nephrosis
Eg Griseofuluin (horses)